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United States Patent | 5,599,820 |
Ojima ,   et al. | February 4, 1997 |
The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.
Inventors: | Ojima; Iwao (Stony Brook, NY); Bombardelli; Ezio (Milan, IT) |
Assignee: | The Research Foundation of State University of New York (Albany, NY); Indena SpA Gruppo Inverni Della Beffa (Milan, IT) |
Appl. No.: | 461730 |
Filed: | June 5, 1995 |
Current U.S. Class: | 514/320; 514/337; 514/422; 514/444; 514/449; 544/131; 544/141; 544/146; 544/147; 544/148; 544/149; 544/152; 546/14; 546/194; 546/196; 546/256; 546/268.1; 546/276.4; 546/278.4; 546/279.1; 546/280.4; 546/281.7; 546/282.1; 546/282.4; 546/283.4; 546/283.7; 546/284.4; 546/284.7; 548/525; 549/60; 549/214; 549/473; 549/510 |
Intern'l Class: | A61K 031/445; A61K 031/21 |
Field of Search: | 549/570,60,473,214 514/449,320,337,422,444 548/525 546/196,269 |
4876399 | Oct., 1989 | Holton et al. | 568/817. |
4924012 | May., 1990 | Colin et al. | 549/510. |
4960790 | Oct., 1990 | Stella et al. | 514/449. |
5015744 | May., 1991 | Holton | 549/510. |
5175315 | Dec., 1992 | Holton | 549/510. |
5264591 | Nov., 1993 | Bombardelli et al. | 549/214. |
5475011 | Dec., 1995 | Ojima et al. | 514/320. |
Foreign Patent Documents | |||
0400971 | May., 1990 | EP. | |
WO9209589 | Jun., 1992 | EP. |
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